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Lowering cholesterol is an important step in preventing and managing heart disease. There are several different types of medications used to treat heart disease and specifically, high cholesterol.

But in addition to the medications you may be familiar with, there are other drugs that may be effective in lowering cholesterol: selective estrogen receptor modulators, used for osteoporosis and to prevent and treat breast cancer, and bile acid binders.

About SERMs

SERMs are medications that have a unique ability. In certain parts of the body — specifically the breasts — they block the effects of the hormone estrogen. This property makes them effective in preventing recurrences of breast cancer after the initial surgery, and in preventing breast cancer in some high-risk women who are likely to get breast cancer in the future.

But SERMs don't stop estrogen's effects everywhere in the body — only in select (hence the name) places.

There are three SERM medications currently available:

Raloxifene (Evista)

Toremifene (Fareston)

Tamoxifen (Nolvadex)

SERMs can also have beneficial effects elsewhere in the body, such as on the bone-thinning disease osteoporosis, where they mimic the helpful effect that estrogen has on the bones. Raloxifene is a SERM primarily prescribed for this purpose.

Pros and Cons of SERMS

Estrogen itself helps to manage the body's production of cholesterol. And at least one SERM, raloxifene, does this too, by lowering LDL (bad) cholesterol and total cholesterol levels. This property of raloxifene is of interest to health researchers for its potential to decrease cardiovascular disease.

A recent study found that women with type 2 diabetes who took raloxifene had less cholesterol and fat in their blood, especially if they weren't taking a statin to treat their high cholesterol.

So while SERMs are busy inhibiting estrogen's effects in the breasts, they are promoting estrogen's effects — building bone and controlling cholesterol — elsewhere in the body. Individual SERMS vary in their ability to do each of these things.

On the downside, SERMs have a number of side effects that can be serious. "There are a couple of problems," says Myron Gerson, MD, cardiologist and professor of medicine and biology at the University of Cincinnati College of Medicine in Ohio. Most concerning is that tamoxifen, in particular, increases the risk of blood clots in the lungs or legs, as well as increasing the risk of stroke. And it can also increase the risk of cancer of the uterus. Raloxifene is less likely to have these effects.

SERMS are not currently prescribed for management of cholesterol, but for those on it for other reasons, such as women on raloxifene for prevention of osteoporosis, it’s a good side effect to have. In a study examining the cholesterol-lowering powers of some SERMs, "the authors suggest intensive reduction in cardiovascular risk by weight reduction, blood pressure control, and statin drugs" rather than through the risky use of SERMs, says Dr. Gerson.

Should You Take Bile Acid Binders?

Bile acid binders, also called resins, are drugs that adhere to bile acids. The liver makes bile acids out of the digested cholesterol. Once the liver converts cholesterol into bile acids, the bile acids make their way into the intestines, where they are absorbed again and sent back to the liver.

Bile acid binders help to lower the “bad” LDL cholesterol, by adhering to these bile acids in the intestines before they return to the liver. This allows the bile acids to be excreted from the body in the feces instead of ending up in the blood. This also encourages the liver to keep turning more and more cholesterol into bile acids, which the body continues to excrete. By converting more cholesterol and ridding itself of the bile acids, the body gets rid of cholesterol — meaning healthier blood cholesterol levels, and less risk of heart disease and heart attack.

Bile acid binders are primarily used to lower cholesterol levels, sometimes in combination with statins, other cholesterol-lowering drugs. One bile acid binder, colesevelam hydrochloride, is also used for controlling blood sugar in people with type 2 diabetes.

Generic and brand names of bile acid binders include:

Colesevelam hydrochloride (Welchol)

Cholestyramine (Questran, Questran Light)

Colestipol (Colestid)

Pros and Cons of Bile Acid Binders

Bile acid binders can be very effective, but even more so when the patient is limiting fat and cholesterol in his diet. Diet control plus bile acid binders can lower cholesterol levels by as much as 15 percent to 20 percent.

The cons: Bile acid binders can be unsafe to take with other medications, as they can interact and cause a serious reaction. In particular, they're known to interact with medications used to treat heart disease, including:

Beta blocker medications for high blood pressure

The blood-thinner warfarin

The heart medication digoxin

Diuretic medications

Diabetes drugs like glyburide and glimepiride

On top of this, bile acid binders can cause various side effects. Side effects can include vitamin deficiencies and annoying gastrointestinal problems, such as constipation and gas. Though rare, some people have experienced serious liver problems, so anyone who has a liver condition should not take a bile acid binder without a doctor's consent.

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